Z705853
Sigma
Analogue-Based Drug Discovery
| ISBN-10: | 3-527-31257-9 |
| ISBN-13: | 978-3-527-31257-3 |
Description
| General description | The easiest way to create a new drug is to modify an existing one. These so-called drug analogs account for about half of all "new" drugs. In addition, drug analogs can be modeled on naturally occurring bioactive substances that do not make good drugs on their own. This first authoritative overview discusses analog-based drug discovery for, among others, beta-blockers, ACE inhibitors, steroids, opiates, coxibs, stigmines, proton pump inhibitors, platinum compounds and quinolones. In addition, case studies on selected commercially successful drug analogs provide prime advice for new drug development projects based on modification. The book has an exclusive table of the 1,000 most successful drug analogs according to IMS ranking, classified in terms of chemical structure, mode of action and patentability. It is officially endorsed by the IUPAC's Drug Development Committee. |
Properties
| publication info | J. Fischer, et al., ed., John Wiley & Sons, 2006, 606 pp., hard cover |
Table Of Contents
| Table of Contents | PART I: GENERAL ASPECTS OF ANALOGUE-BASED DRUG DISCOVERY. 1. Analogues as a Means of Discovering New Drugs. 2. Drug Likeness and Analogue-Based Drug Discovery. 3. Privileged Structures and Analog-Based Drug Discovery. PART II: SELECTED EXAMPLES FROM THE ANALOGUE-BASED DRUG DISCOVERIES. 1. Development of Anti-Ulcer H2-Receptor Histamine Antagonists. 2. Esomeprazole in the Framework of Proton-Pump Inhibitor Development. 3. The Development of a New Proton-Pump Inhibitor: The Case History of Pantoprazole. 4. Optimizing the Clinical Pharmacologic Properties of the HMG-CoA Reductase Inhibitors. 5. Optimizing Antihypertensive Therapy by Angiotensin Receptor Blockers. 6. Optimizing Antihypertensive Therapy by Angiotensin-Converting Enzyme Inhibitors. 7. Case Study of Lacidipine in the Research of New Calcium Antagonists. 8. Selective Beta-Adrenergic Receptor-Blocking Agents. 9. Case Study: "Esmolol Stat". 10. Development of Organic Nitrates for Coronary Heart Disease. 11. Development of Opioid Receptor Ligands. 12. Stigmines. 13. Structural Analogues of Clozapine. 14. Quinolone Antibiotics: The Development of Moxifloxacin. 15. The Development of Bisphosphonates as Drugs. 16. Cisplatin and its Analogs for Cancer Chemotherapy. 17. The History of Drospirenone. 18. Histamine H1 Blockers: From Relative Failures to Blockbusters Within Series of Analogues. 19. Corticosteroids: From Natural Products to Useful Analogues. PART III: TABLE OF SELECTED ANALOGUE CLASSES. Index. |
